WO2011059969A3 - Mammalian metabolites of steroids - Google Patents

Mammalian metabolites of steroids Download PDF

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Publication number
WO2011059969A3
WO2011059969A3 PCT/US2010/055996 US2010055996W WO2011059969A3 WO 2011059969 A3 WO2011059969 A3 WO 2011059969A3 US 2010055996 W US2010055996 W US 2010055996W WO 2011059969 A3 WO2011059969 A3 WO 2011059969A3
Authority
WO
WIPO (PCT)
Prior art keywords
steroids
compounds
methods
mammalian metabolites
metabolites
Prior art date
Application number
PCT/US2010/055996
Other languages
French (fr)
Other versions
WO2011059969A2 (en
Inventor
Scott C. Chappel
David S. Casebier
Original Assignee
Tokai Pharmaceuticals, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tokai Pharmaceuticals, Inc. filed Critical Tokai Pharmaceuticals, Inc.
Priority to JP2012538889A priority Critical patent/JP5956928B2/en
Priority to CN201080059467.3A priority patent/CN102822190B/en
Priority to EP10830591A priority patent/EP2499151A4/en
Priority to US13/508,726 priority patent/US20120282331A1/en
Priority to CA2780365A priority patent/CA2780365A1/en
Priority to AU2010319697A priority patent/AU2010319697B2/en
Priority to BR112012012167A priority patent/BR112012012167A2/en
Publication of WO2011059969A2 publication Critical patent/WO2011059969A2/en
Publication of WO2011059969A3 publication Critical patent/WO2011059969A3/en
Priority to US15/273,121 priority patent/US20170008920A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Abstract

Described herein, in certain embodiments, are steroidal derivatives, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions.
PCT/US2010/055996 2009-11-13 2010-11-09 Mammalian metabolites of steroids WO2011059969A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
JP2012538889A JP5956928B2 (en) 2009-11-13 2010-11-09 Mammalian steroid metabolites
CN201080059467.3A CN102822190B (en) 2009-11-13 2010-11-09 Mammiferous steroid metabolism thing
EP10830591A EP2499151A4 (en) 2009-11-13 2010-11-09 Mammalian metabolites of steroids
US13/508,726 US20120282331A1 (en) 2009-11-13 2010-11-09 Mammalian metabolites of steroids
CA2780365A CA2780365A1 (en) 2009-11-13 2010-11-09 Mammalian metabolites of steroids
AU2010319697A AU2010319697B2 (en) 2009-11-13 2010-11-09 Mammalian metabolites of steroids
BR112012012167A BR112012012167A2 (en) 2009-11-13 2010-11-09 MAMMALIAN STEROID METABOLITES
US15/273,121 US20170008920A1 (en) 2009-11-13 2016-09-22 Mammalian metabolites of steroids

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26126209P 2009-11-13 2009-11-13
US61/261,262 2009-11-13

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/508,726 A-371-Of-International US20120282331A1 (en) 2009-11-13 2010-11-09 Mammalian metabolites of steroids
US15/273,121 Continuation US20170008920A1 (en) 2009-11-13 2016-09-22 Mammalian metabolites of steroids

Publications (2)

Publication Number Publication Date
WO2011059969A2 WO2011059969A2 (en) 2011-05-19
WO2011059969A3 true WO2011059969A3 (en) 2011-09-22

Family

ID=43992357

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/055996 WO2011059969A2 (en) 2009-11-13 2010-11-09 Mammalian metabolites of steroids

Country Status (8)

Country Link
US (2) US20120282331A1 (en)
EP (1) EP2499151A4 (en)
JP (1) JP5956928B2 (en)
CN (1) CN102822190B (en)
AU (1) AU2010319697B2 (en)
BR (1) BR112012012167A2 (en)
CA (1) CA2780365A1 (en)
WO (1) WO2011059969A2 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100047338A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
US20110312916A1 (en) 2009-02-05 2011-12-22 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
AU2010264698C1 (en) 2009-06-26 2013-05-16 Novartis Ag 1, 3-disubstituted imidazolidin-2-one derivatives as inhibitors of CYP 17
AU2012249421B9 (en) 2011-04-28 2015-10-22 Novartis Ag 17alpha-hydroxylase/C17,20-lyase inhibitors
EP4066841A1 (en) 2013-03-14 2022-10-05 University of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
CN105636594A (en) 2013-08-12 2016-06-01 托凯药业股份有限公司 Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
US10675289B2 (en) 2014-10-02 2020-06-09 University Of Maryland, Baltimore Methods of treating pancreatic cancer
WO2016119742A1 (en) * 2015-01-29 2016-08-04 苏州晶云药物科技有限公司 (3β)-17-(1h-benzimidazole-1-yl)androstane-5, and 16-diene-3-ol salts and preparation methods therefor
WO2017140183A1 (en) * 2016-02-19 2017-08-24 深圳市塔吉瑞生物医药有限公司 Substituted steroids and use thereof
CN111454315B (en) * 2020-04-15 2022-12-09 宁波第二激素厂 Synthesis method of androstane-16-alkene-3 beta-alcohol

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006093993A1 (en) * 2005-03-02 2006-09-08 University Of Maryland Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity

Family Cites Families (6)

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Publication number Priority date Publication date Assignee Title
US3480621A (en) * 1967-01-17 1969-11-25 Phytogen Prod Inc Steroid ketal
ES2138618T3 (en) * 1992-03-31 2000-01-16 Btg Int Ltd STEROIDS 17-SUBSTITUTED USEFUL IN THE TREATMENT OF CANCER.
DE4232681C2 (en) * 1992-09-29 1994-11-24 Sigma Tau Ind Farmaceuti 17-phenyl and 17-furyl-14beta, 5alpha-androstane and androsten derivatives, processes for their preparation and pharmaceutical composition containing them
GB2470873A (en) * 2008-03-12 2010-12-08 Univ Maryland Androgen receptor inactivation contributes to antitumor efficacy of CYP17 inhibitors in prostrate cancer
US20110118219A1 (en) * 2008-03-25 2011-05-19 University Of Maryland, Baltimore Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
US20110319369A1 (en) * 2009-02-05 2011-12-29 Tokai Pharmaceuticals, Inc. Combination of a 17 alpha-hydroxylase/c17, 20-lyase inhibitor with an additional therapeutic agent

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006093993A1 (en) * 2005-03-02 2006-09-08 University Of Maryland Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
HAKKI T. ET AL: "CYP17- and CYP11B-dependent steroid hydroxylases as drug development targets", PHARMACOLOGY & THERAPEUTICS, vol. 111, July 2006 (2006-07-01), pages 27 - 52, XP025038482, DOI: doi:10.1016/j.pharmthera.2005.07.006 *
HANDRATTA V.D. ET AL: "Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens: Synthesis, in Vitro Biological Activity, Pharmacokinetics, and Antitumor Activity in the LAPC4 Human Prostate Cancer Xenograft Model", JOUR NAL OF MEDICINAL CHEMISTRY, vol. 48, 21 April 2005 (2005-04-21), pages 2972 - 2984, XP002535274, DOI: doi:10.1021/JM040202W *
VASAITIS T. ET AL: "Androgen receptor inactivation contributes to antitumor efficacy of 17alpha-hydroxylase/17,20-lyase inhibitor 3beta-hydroxy-17-(lH-benzimidazole-l-yl)androst a-5,16-diene in prostate cancer", MOLECULAR CANCER THERAPEUTICS, vol. 7, August 2008 (2008-08-01), pages 2348 - 2357, XP008152075, DOI: doi:10.1158/1535-7163.MCT-08-0230 *

Also Published As

Publication number Publication date
CA2780365A1 (en) 2011-05-19
AU2010319697B2 (en) 2016-05-19
WO2011059969A2 (en) 2011-05-19
US20120282331A1 (en) 2012-11-08
AU2010319697A1 (en) 2012-06-07
EP2499151A4 (en) 2013-03-20
JP5956928B2 (en) 2016-07-27
CN102822190B (en) 2016-03-30
US20170008920A1 (en) 2017-01-12
EP2499151A2 (en) 2012-09-19
JP2013510856A (en) 2013-03-28
CN102822190A (en) 2012-12-12
BR112012012167A2 (en) 2017-10-03

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